903565-83-3Relevant articles and documents
Synthesis of Tofogliflozin as an SGLT2 Inhibitor via Construction of Dihydroisobenzofuran by Intramolecular [4 + 2] Cycloaddition
Murakata, Masatoshi,Kawase, Akira,Kimura, Nobuaki,Ikeda, Takuma,Nagase, Masahiro,Koizumi, Masatoshi,Kuwata, Kazuaki,Maeda, Kenji,Shimizu, Hitoshi
, p. 548 - 557 (2019/03/07)
The synthesis of tofogliflozin (1), a sodium glucose cotransporter 2 (SGLT2) inhibitor, was achieved through the key steps of intramolecular [4 + 2] cycloaddition of dienone-yne intermediate, aerobic aromatization, and anomeric equilibration, thus enablin
Preparation method of Tofogliflozin monohydrate
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Paragraph 0049; 0050; 0051, (2017/06/19)
The invention relates to a preparation method of Tofogliflozin monohydrate. In the route, p-Hydroxybenzoic acid used as a starting material is subjected to acylation, iodination, Friedel-Crafts and reduction reaction to obtain an iodinated diphenylmethane framework; by means of the characteristic that an iodinated substance is reactive, the splicing the diphenylmethane framework and a saccharide ring is realized under mild conditions through the effect of isopropyl magnesium chloride lithium chloride; and the eleven-step total yield is 22%. The route is high in yield, favorable in selectivity, low in production cost and mild in reaction conditions, does not use flammable, explosive or high-toxicity reagent, obtains products and intermediate compounds which are easy to purify, and is suitable for industrial production.
Method for preparing derivatives of spiroketal
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, (2016/10/07)
Provided is a process for the preparation of a spiroketal derivative via a compound represented by general formula (II) [wherein each variable group and each variable number are as defined in the description].